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**Camostat mesilate** is an orally active synthetic small-molecule, broad-spectrum serine protease inhibitor and the mesilate salt of camostat. It was originally developed by Ono Pharmaceutical and is marketed in Japan as **Foipan** for remission of acute symptoms of chronic pancreatitis and for postoperative reflux esophagitis. Camostat inhibits digestive, coagulation, fibrinolytic, and cell-surface serine proteases, including trypsin, plasma kallikrein, plasmin, thrombin, and transmembrane protease serine 2. Its inhibition of transmembrane protease serine 2 can block spike-protein priming required for cell entry by SARS-CoV-2, which led to extensive COVID-19 repurposing studies; however, it is not approved for COVID-19. Camostat is rapidly converted in vivo to active metabolites including 4-(4-guanidinobenzoyloxy)phenylacetic acid. Beyond its established gastrointestinal indications, it has been evaluated in chronic kidney disease, cystic fibrosis, protein-losing enteropathy after Fontan operation, obesity, and COVID-19.
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